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Assay Detail

CHEMBL1056701

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Functional
Agonist activity at human PPARalpha expressed in african green monkey COS7 cells by Gal4 transactivation assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Peroxisome proliferator-activated receptor alpha (CHEMBL239)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a novel class of 2-mercaptohexanoic acid derivatives as highly active PPARalpha agonists.
Zettl H, Steri R, Lämmerhofer M, Schubert-Zsilavecz M.
Bioorg Med Chem Lett (2009) 19 : 4421 -4426
PubMed 19556125 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 6.66 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL551479 1 7.96
CHEMBL561544 1 7.68
CHEMBL564017 1 7.60
CHEMBL550332 1 7.31
CHEMBL558141 1 7.25
CHEMBL557342 1 7.07
CHEMBL560484 1 7.05
CHEMBL563351 1 6.96
CHEMBL563546 1 6.82
CHEMBL558072 1 6.72
CHEMBL551420 1 6.66
CHEMBL549723 1 6.60
CHEMBL552347 1 6.54
CHEMBL551884 1 6.41
CHEMBL560205 1 6.26
CHEMBL562786 1 6.22
CHEMBL559752 1 5.82
CHEMBL551480 1 5.77
CHEMBL561284 1 5.70
CHEMBL561006 1 4.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL551479 EC50 = 11.0 nM 7.96
CHEMBL561544 EC50 = 21.0 nM 7.68
CHEMBL564017 EC50 = 25.0 nM 7.60
CHEMBL550332 EC50 = 49.0 nM 7.31
CHEMBL558141 EC50 = 56.0 nM 7.25
CHEMBL557342 EC50 = 85.0 nM 7.07
CHEMBL560484 EC50 = 90.0 nM 7.05
CHEMBL563351 EC50 = 110.0 nM 6.96
CHEMBL563546 EC50 = 150.0 nM 6.82
CHEMBL558072 EC50 = 190.0 nM 6.72
CHEMBL551420 EC50 = 220.0 nM 6.66
CHEMBL549723 EC50 = 250.0 nM 6.60
CHEMBL552347 EC50 = 290.0 nM 6.54
CHEMBL551884 EC50 = 390.0 nM 6.41
CHEMBL560205 EC50 = 550.0 nM 6.26
CHEMBL562786 EC50 = 600.0 nM 6.22
CHEMBL559752 EC50 = 1500.0 nM 5.82
CHEMBL551480 EC50 = 1700.0 nM 5.77
CHEMBL561284 EC50 = 2000.0 nM 5.70
CHEMBL561006 EC50 = 13800.0 nM 4.86